WO2011086099A1 - Novel substituted triazole derivatives as gamma secretase modulators - Google Patents

Novel substituted triazole derivatives as gamma secretase modulators Download PDF

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Publication number
WO2011086099A1
WO2011086099A1 PCT/EP2011/050350 EP2011050350W WO2011086099A1 WO 2011086099 A1 WO2011086099 A1 WO 2011086099A1 EP 2011050350 W EP2011050350 W EP 2011050350W WO 2011086099 A1 WO2011086099 A1 WO 2011086099A1
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WO
WIPO (PCT)
Prior art keywords
halo
substituents
hydrogen
alkyl
optionally substituted
Prior art date
Application number
PCT/EP2011/050350
Other languages
English (en)
French (fr)
Inventor
Sven Franciscus Anna Van Brandt
Michel Anna Jozef De Cleyn
Henricus Jacobus Maria Gijsen
Didier Jean-Claude Berthelot
Michel Surkyn
Original Assignee
Ortho-Mcneil-Janssen Pharmaceuticals, Inc
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Priority to EP11700832.6A priority Critical patent/EP2523949B1/en
Priority to EA201290654A priority patent/EA022093B1/ru
Priority to JP2012548423A priority patent/JP5824464B2/ja
Priority to CN2011800059936A priority patent/CN102906083A/zh
Priority to MX2012008260A priority patent/MX2012008260A/es
Priority to US13/522,409 priority patent/US9079886B2/en
Priority to UAA201207267A priority patent/UA109776C2/ru
Application filed by Ortho-Mcneil-Janssen Pharmaceuticals, Inc filed Critical Ortho-Mcneil-Janssen Pharmaceuticals, Inc
Priority to KR1020127020510A priority patent/KR20130028048A/ko
Priority to AU2011206635A priority patent/AU2011206635B2/en
Priority to SG2012051694A priority patent/SG182506A1/en
Priority to ES11700832.6T priority patent/ES2523977T3/es
Priority to BR112012017310A priority patent/BR112012017310A2/pt
Priority to CA2784769A priority patent/CA2784769A1/en
Priority to NZ600648A priority patent/NZ600648A/en
Publication of WO2011086099A1 publication Critical patent/WO2011086099A1/en
Priority to IL220838A priority patent/IL220838A0/en
Priority to ZA2012/05240A priority patent/ZA201205240B/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
PCT/EP2011/050350 2010-01-15 2011-01-12 Novel substituted triazole derivatives as gamma secretase modulators WO2011086099A1 (en)

Priority Applications (16)

Application Number Priority Date Filing Date Title
KR1020127020510A KR20130028048A (ko) 2010-01-15 2011-01-12 감마 세크레타제 조절제로서의 신규 치환된 트리아졸 유도체
AU2011206635A AU2011206635B2 (en) 2010-01-15 2011-01-12 Novel substituted triazole derivatives as gamma secretase modulators
EA201290654A EA022093B1 (ru) 2010-01-15 2011-01-12 Замещенные триазольные производные как модуляторы гамма-секретазы
SG2012051694A SG182506A1 (en) 2010-01-15 2011-01-12 Novel substituted triazole derivatives as gamma secretase modulators
MX2012008260A MX2012008260A (es) 2010-01-15 2011-01-12 Novedosos derivados de triazol sustituidos como moduladores de la gamma secretasa.
US13/522,409 US9079886B2 (en) 2010-01-15 2011-01-12 Substituted triazole derivatives as gamma secretase modulators
UAA201207267A UA109776C2 (ru) 2010-01-15 2011-01-12 Замещенные триазольные производные как модуляторы гамма-секретазы
EP11700832.6A EP2523949B1 (en) 2010-01-15 2011-01-12 Novel substituted triazole derivatives as gamma secretase modulators
NZ600648A NZ600648A (en) 2010-01-15 2011-01-12 Novel substituted triazole derivatives as gamma secretase modulators
JP2012548423A JP5824464B2 (ja) 2010-01-15 2011-01-12 γセクレターゼ調節物質としての新規置換トリアゾール誘導体
CN2011800059936A CN102906083A (zh) 2010-01-15 2011-01-12 作为γ分泌酶调节剂的新的取代的三唑衍生物
ES11700832.6T ES2523977T3 (es) 2010-01-15 2011-01-12 Derivados de triazol sustituidos novedosos como moduladores de gamma secretasa
BR112012017310A BR112012017310A2 (pt) 2010-01-15 2011-01-12 derivados de triazol substituídos como moduladores de gama secretase
CA2784769A CA2784769A1 (en) 2010-01-15 2011-01-12 Novel substituted triazole derivatives as gamma secretase modulators
IL220838A IL220838A0 (en) 2010-01-15 2012-07-10 Novel substituted triazole derivatives as gamma secretase modulators
ZA2012/05240A ZA201205240B (en) 2010-01-15 2012-07-13 Novel substituted triazole derivatives as gamma secretase modulators

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP10150892 2010-01-15
EP10150892.7 2010-01-15
EP10171292.5 2010-07-29
EP10171292 2010-07-29

Publications (1)

Publication Number Publication Date
WO2011086099A1 true WO2011086099A1 (en) 2011-07-21

Family

ID=43569255

Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/EP2011/050350 WO2011086099A1 (en) 2010-01-15 2011-01-12 Novel substituted triazole derivatives as gamma secretase modulators
PCT/EP2011/050349 WO2011086098A1 (en) 2010-01-15 2011-01-12 Novel substituted bicyclic triazole derivatives as gamma secretase modulators

Family Applications After (1)

Application Number Title Priority Date Filing Date
PCT/EP2011/050349 WO2011086098A1 (en) 2010-01-15 2011-01-12 Novel substituted bicyclic triazole derivatives as gamma secretase modulators

Country Status (20)

Country Link
US (2) US9145399B2 (ru)
EP (2) EP2523949B1 (ru)
JP (2) JP5824464B2 (ru)
KR (2) KR20120123677A (ru)
CN (2) CN102906083A (ru)
AR (2) AR079904A1 (ru)
AU (2) AU2011206635B2 (ru)
BR (2) BR112012017310A2 (ru)
CA (2) CA2784765A1 (ru)
CL (2) CL2012001955A1 (ru)
EA (2) EA021776B1 (ru)
ES (2) ES2523977T3 (ru)
IL (2) IL220838A0 (ru)
MX (2) MX2012008259A (ru)
NZ (2) NZ600648A (ru)
PE (2) PE20121511A1 (ru)
SG (2) SG182505A1 (ru)
TW (2) TWI491608B (ru)
WO (2) WO2011086099A1 (ru)
ZA (2) ZA201205240B (ru)

Cited By (23)

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WO2013124026A1 (en) * 2012-02-21 2013-08-29 Merck Patent Gmbh 8 - substituted 2 -amino - [1,2,4] triazolo [1, 5 -a] pyrazines as syk tryrosine kinase inhibitors and gcn2 serin kinase inhibitors
JP2013538214A (ja) * 2010-08-27 2013-10-10 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング トリアゾロピラジン誘導体
US8835482B2 (en) 2009-05-07 2014-09-16 Janssen Pharmaceuticals, Inc. Substituted indazole and aza-indazole derivatives as gamma secretase modulators
WO2014195323A1 (en) 2013-06-04 2014-12-11 Acturum Life Science AB Pyrimidine compounds and their use as gamma secretase modulators
WO2014195322A1 (en) 2013-06-04 2014-12-11 Acturum Life Science AB Triazole compounds and their use as gamma secretase modulators
US8946266B2 (en) 2009-07-15 2015-02-03 Janssen Pharmaceuticals, Inc. Substituted triazole and imidazole derivatives as gamma secretase modulators
US8946426B2 (en) 2009-02-06 2015-02-03 Janssen Pharmaceuticals, Inc. Substituted bicyclic heterocyclic compounds as gamma secretase modulators
CN104428289A (zh) * 2012-07-06 2015-03-18 弗·哈夫曼-拉罗切有限公司 作为抗病毒剂的三唑化合物
US8987276B2 (en) 2011-03-24 2015-03-24 Janssen Pharmaceuticals, Inc. Substituted triazolyl piperazine and triazolyl piperidine derivatives as gamma secretase modulators
US9079886B2 (en) 2010-01-15 2015-07-14 Janssen Pharmaceuticals, Inc. Substituted triazole derivatives as gamma secretase modulators
US9115143B2 (en) 2011-07-15 2015-08-25 Janssen Pharmaceuticals, Inc. Substituted indole derivatives as gamma secretase modulators
US9181245B2 (en) 2012-05-16 2015-11-10 Janssen Pharmaceuticals, Inc. Substituted pyrido[1,2-a]pyrazines and substituted pyrido[1,2-a][1,4]diazepines for the treatment of (inter alia) Alzheimer's disease
US9512126B2 (en) 2012-03-14 2016-12-06 Bayer Intellectual Property Gmbh Substituted imidazopyridazines
US9555022B2 (en) 2010-06-16 2017-01-31 Bayer Intellectual Property Gmbh Substituted triazolopyridines
US9586958B2 (en) 2013-06-11 2017-03-07 Bayer Pharma Aktiengesellschaft Prodrug derivatives of substituted triazolopyridines
US9611254B2 (en) 2013-06-04 2017-04-04 Acturum Life Science AB Triazole compounds and their use as gamma secretase modulators
US9663510B2 (en) 2011-12-12 2017-05-30 Bayer Pharma Aktiengesellschaft Substituted triazolopyridines and their use as TTK inhibitors
US9676766B2 (en) 2009-11-30 2017-06-13 Bayer Intellectual Property Gmbh Triazolopyridines
US10112943B2 (en) 2012-12-20 2018-10-30 Janssen Pharmaceutica Nv Substituted imidazoles as gamma secretase modulators
US10246454B2 (en) 2013-01-17 2019-04-02 Janssen Pharmaceutica Nv Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators
CN110194744A (zh) * 2018-02-26 2019-09-03 云南大学 一种抑制β-淀粉样蛋白生成的化合物及其制备方法和用途
CN110194743A (zh) * 2018-02-26 2019-09-03 云南大学 苯基(3-甲氧基-4-(4-甲基-1h-咪唑-1-基)苯基)甲酮类化合物
US10562897B2 (en) 2014-01-16 2020-02-18 Janssen Pharmaceutica Nv Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators

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CN103508957B (zh) * 2012-06-25 2017-02-08 中国科学院上海药物研究所 羟乙基吡唑类化合物或氨乙基吡唑类化合物及其制备方法和用途
EP2687528A1 (en) 2012-07-17 2014-01-22 Ares Trading S.A. Fused triazole derivatives as gamma secretase modulators
JOP20180012A1 (ar) * 2012-08-07 2019-01-30 Janssen Pharmaceutica Nv عملية السلفنة باستخدام نونافلوروبوتانيسولفونيل فلوريد
CN107249580A (zh) 2014-12-05 2017-10-13 An2H探索有限公司 帕金连接酶活化方法和组合物
KR101594470B1 (ko) 2015-05-28 2016-02-16 주식회사 네비엔 프리캐스트 콘크리트 슬래브 및 이들의 결합구조
KR101710943B1 (ko) 2016-05-13 2017-02-28 강태성 구조물용 피씨 데크 슬래브 및 이의 제조방법
CA3066110A1 (en) 2016-06-03 2017-12-07 An2H Discovery Limited Triazole benzamide derivatives and the compositions and methods of treatment regarding the same
EP3475279B1 (en) * 2016-06-27 2021-07-14 F. Hoffmann-La Roche AG Triazolopyridines as gamma-secretase modulators
CN109415369B (zh) 2016-07-08 2021-12-07 豪夫迈·罗氏有限公司 稠合嘧啶衍生物
CN109476670B (zh) * 2016-10-04 2022-06-28 豪夫迈·罗氏有限公司 二环杂芳基衍生物
WO2018087018A1 (en) 2016-11-08 2018-05-17 F. Hoffmann-La Roche Ag Phenoxytriazoles
US10889553B2 (en) 2017-12-01 2021-01-12 Nysnobio Ireland Dac Asymmetric triazole benzamide derivatives and the compositions and methods of treatment regarding the same
CN110194746B (zh) * 2018-02-26 2022-11-18 云南大学 用于治疗阿尔茨海默症的化合物，其制备方法和用途
US20230048657A1 (en) 2019-11-29 2023-02-16 Hoffmann-La Roche Inc. Process for the preparation of (9s)-2-bromo-9-(2,3,4-trifluorophenyl)-6,7,8,9-tetrahydro-5h-[1,2,4]triazolo[1,5-a]azepine
AR124194A1 (es) 2020-12-11 2023-02-22 Hoffmann La Roche Proceso para la preparación de (9s)-n-[3-(6-metilpirimidin-4-il)-3-azabiciclo[3.2.1]octan-8-il]-9-(2,3,4-trifluorofenil)-6,7,8,9-tetrahidro-5h-[1,2,4]triazolo[1,5-a]azepin-2-amina y su forma sólida

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